olmutinib

Olmutinib is an orally active, third-generation small molecule epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor developed for the treatment of non-small cell lung cancer (NSCLC) harboring the T790M mutation in EGFR. It selectively and irreversibly binds to a cysteine residue near the kinase domain of mutant EGFRs, inhibiting phosphorylation and downstream signaling pathways that promote tumor cell survival and proliferation. Olmutinib shows minimal activity against wild-type EGFR. The drug was originally developed by Hanmi Pharmaceutical and Boehringer Ingelheim. It received breakthrough therapy designation in the United States in December 2015 for NSCLC with T790M mutation and was approved in South Korea in May 2016 as a second-line treatment for this indication[1][2][4][5]. Resistance to olmutinib has been reported due to secondary mutations such as C797S[2]. The drug has also demonstrated activity reversing multidrug resistance mediated by ABCG2 transporters[6].

Brand names

Olita

Other names

1353550-13-61802181-20-9